Increasing effect of sodium 3-ethyl-7-isopropyl-1-azulenesulfonate 1/3 hydrate (KT1-32), a novel antiulcer agent, on gastric mucosal blood flow in anesthetized.
Effect of a novel azulene derivative KT1-32 on gastric mucosal blood flow (GMBF) was studied to elucidate its mucosal defensive mechanisms underlying the antiulcer action. The GMBF was measured by two methods which were based on heat clearance and laser Doppler velocimetry in the rat. Intravenous administration of KT1-32 produced a dose-dependent increase in GMBF at doses of 0.3-10 mg/kg; significant increases in GMBF were observed at doses not less than 1 or 3 mg/kg by the laser Doppler or heat clearance method, respectively. The duration of action was about 10 min at 10 mg/kg of KT1-32. A good parallelism in these GMBF changes was noted between both methods. Cetraxate, an antiulcer agent, elicited an increase in GMBF at 30 mg/kg, i.v., when GMBF was measured by the heat clearance method. Sodium guaiazulene 3-sulfonate, another azulene antiulcer agent, showed no increase in GMBF. It is suggested that the increasing effect of KT1-32 on GMBF contributes to its antiulcer activity through strengthening mucosal defensive mechanisms.
Yano
S
S
Department of Drug Evaluation and Toxicological Sciences, Faculty of Pharmaceutical Sciences, Chiba University, Japan.
Horie
S
S
Wakabayashi
S
S
Mochizuki
S
S
Tomiyama
A
A
Watanabe
K
K
D000758:Anesthesia; D000818:Animals; D000897:Anti-Ulcer Agents / Q000494:pharmacology*; D052176:Azulenes; D005753:Gastric Mucosa / Q000098:blood supply* / Q000187:drug effects; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D012039:Regional Blood Flow / Q000187:drug effects; D012717:Sesquiterpenes / Q000494:pharmacology*
D000897:Anti-Ulcer Agents; D052176:Azulenes; D012717:Sesquiterpenes; C061956:azuletil